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. Author manuscript; available in PMC: 2019 Feb 19.
Published in final edited form as: Bioorg Med Chem. 2018 Mar 19;26(11):2984–2991. doi: 10.1016/j.bmc.2018.03.030

Table 3.

AlphaScreen IC50 values for displacement of H3K4me3-Bn from His-KDM7(PHD) by AMI derivatives. Final concentrations of protein and H3K4me3-Bn were: 6.25 nM KDM7A(PHD) and 25 nM peptide, 12.5 nM each for KDM7B(PHD), and 25 nM KDM7C(PHD) and 6.25 nM peptide. Average ± StdDev (n ≥ 3 independent replicates) shown.

IC50 (μM)
Compounds KDM7A(PHD) KDM7B(PHD) KDM7C(PHD)
AMI 156 ± 12 252 ± 53 84 ± 14
WAG-003 2232 ± 790 307 ± 76 976 ± 146
WAG-005 50 ± 5 390 ± 158 740 ± 149
1a 333 ± 39 397 ± 77 158 ± 30
2a 8 ± 9 355 ± 39 579 ± 87
2b 108 ± 15 310 ± 78 598 ± 119
2c 104 ± 8 377 ± 76 501 ± 75
2d 98 ± 10 697 ± 154 682 ± 97
7a 102 ± 15 496 ± 181 1294 ± 280
7b 326 ± 14 286 ± 84 533 ± 99
8a 76 ± 14 240 ± 58 228 ± 66
8b 68 ± 13 242 ± 41 220 ± 40
10 534 ± 150 386 ± 41 359 ± 89
12 151 ± 17 221 ± 57 334 ± 45